7 strategies to improve PROTACs’ oral bioavailability¬†

[PROTAC image courtesy of Wikipedia]

PROteolysis TArgeting Chimera (PROTAC)* drugs emerged in 2001 as a novel therapeutic option for treating previously untreatable diseases. To date, no PROTAC drugs have earned U.S. FDA approval, but the technology has opened up a promising new chapter in drug discovery. PROTACs are being widely explored across both industry and academia and have expanded from treating cancer to immune disorders, neurodegenerative diseases, viral infections, etc.

A PROTAC molecule consists of three components: a ligand binding to a target protein, a ligand binding to E3 ligase and a linker. Unlike conventional small molecules that block target proteins via inhibition, PROTACs bind specifically to target proteins and induce their degradation by leveraging the ubiquitin-proteasome system (UPS). PROTACs’ binding process is referred to as a “chemical knockdown” approach.

PR…

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Unlock advanced CBD formulations with nutritional lipids

Scientist pipetting samples into micro centrifuge tubes ready for automated analysis. Image courtesy of DSM.

Cannabidiol (CBD) is fast emerging as an exciting ingredient across the pharmaceutical market, powered by increasing scientific research investigating its potential benefits in a number of disease states, including central nervous system (CNS) disorders, pain management, cancer and more. While there is a remarkable opportunity for the development of CBD-based solutions in the field, formulation can be challenging at times, especially when the focus is on increasing the oral bioavailability of the molecule. There are new and emerging ways to address the technical challenges associated with CBD bioavailability and enable the molecule to fulfill its full potential as a therapeutic agent. Here, we explore how lipid-based systems may hold the key to success in this space.

Understanding the complexity of CBD f…
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